US8431585B2 - Use of inhibitors of the EGFR-mediated signal transduction for the treatment of benign prostatic hyperplasia (BPH)/prostatic hypertrophy - Google Patents

Use of inhibitors of the EGFR-mediated signal transduction for the treatment of benign prostatic hyperplasia (BPH)/prostatic hypertrophy Download PDF

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Publication number
US8431585B2
US8431585B2 US12/706,819 US70681910A US8431585B2 US 8431585 B2 US8431585 B2 US 8431585B2 US 70681910 A US70681910 A US 70681910A US 8431585 B2 US8431585 B2 US 8431585B2
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Prior art keywords
amino
group
quinazoline
chloro
fluorophenyl
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Expired - Lifetime, expires
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US12/706,819
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English (en)
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US20100144639A1 (en
Inventor
Thomas Singer
Stefan Platz
Florian Colbatzky
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Boehringer Ingelheim Pharma GmbH and Co KG
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Boehringer Ingelheim Pharma GmbH and Co KG
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Priority claimed from US10/431,699 external-priority patent/US20030225079A1/en
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Priority to US12/706,819 priority Critical patent/US8431585B2/en
Publication of US20100144639A1 publication Critical patent/US20100144639A1/en
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
US12/706,819 2002-05-11 2010-02-17 Use of inhibitors of the EGFR-mediated signal transduction for the treatment of benign prostatic hyperplasia (BPH)/prostatic hypertrophy Expired - Lifetime US8431585B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US12/706,819 US8431585B2 (en) 2002-05-11 2010-02-17 Use of inhibitors of the EGFR-mediated signal transduction for the treatment of benign prostatic hyperplasia (BPH)/prostatic hypertrophy

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
DE10221018 2002-05-11
DE10221018A DE10221018A1 (de) 2002-05-11 2002-05-11 Verwendung von Hemmern der EGFR-vermittelten Signaltransduktion zur Behandlung von gutartiger Prostatahyperplasie (BPH)/Prostatahypertrophie
US38981502P 2002-06-18 2002-06-18
US10/431,699 US20030225079A1 (en) 2002-05-11 2003-05-08 Use of inhibitors of the EGFR-mediated signal transduction for the treatment of benign prostatic hyperplasia (BPH)/prostatic hypertrophy
US11/609,407 US20070099918A1 (en) 2002-05-11 2006-12-12 Use of inhibitors of the EGFR-mediated signal transduction for the treatment of benign prostatic hyperplasia (BPH) / prostatic hypertrophy
US12/706,819 US8431585B2 (en) 2002-05-11 2010-02-17 Use of inhibitors of the EGFR-mediated signal transduction for the treatment of benign prostatic hyperplasia (BPH)/prostatic hypertrophy

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
US11/609,407 Continuation US20070099918A1 (en) 2002-05-11 2006-12-12 Use of inhibitors of the EGFR-mediated signal transduction for the treatment of benign prostatic hyperplasia (BPH) / prostatic hypertrophy

Publications (2)

Publication Number Publication Date
US20100144639A1 US20100144639A1 (en) 2010-06-10
US8431585B2 true US8431585B2 (en) 2013-04-30

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Family Applications (1)

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US12/706,819 Expired - Lifetime US8431585B2 (en) 2002-05-11 2010-02-17 Use of inhibitors of the EGFR-mediated signal transduction for the treatment of benign prostatic hyperplasia (BPH)/prostatic hypertrophy

Country Status (11)

Country Link
US (1) US8431585B2 (de)
EP (1) EP1505981B1 (de)
JP (1) JP4630659B2 (de)
AR (1) AR039987A1 (de)
AU (1) AU2003233223A1 (de)
CA (1) CA2483590C (de)
DE (1) DE10221018A1 (de)
PE (1) PE20040400A1 (de)
TW (1) TW200407147A (de)
UY (1) UY27800A1 (de)
WO (1) WO2003094921A2 (de)

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US7019012B2 (en) * 2000-12-20 2006-03-28 Boehringer Ingelheim International Pharma Gmbh & Co. Kg Quinazoline derivatives and pharmaceutical compositions containing them
DE10221018A1 (de) 2002-05-11 2003-11-27 Boehringer Ingelheim Pharma Verwendung von Hemmern der EGFR-vermittelten Signaltransduktion zur Behandlung von gutartiger Prostatahyperplasie (BPH)/Prostatahypertrophie
US20050043233A1 (en) * 2003-04-29 2005-02-24 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
DE10349113A1 (de) 2003-10-17 2005-05-12 Boehringer Ingelheim Pharma Verfahren zur Herstellung von Aminocrotonylverbindungen
GEP20084551B (en) * 2004-05-06 2008-11-25 Warner Lambert Co 4-phenylamino-quinazolin-6-yl-amides
EP1948180B1 (de) * 2005-11-11 2013-03-13 Boehringer Ingelheim International GmbH Kombinationsbehandlung gegen krebs mit egfr/her2-hemmern
WO2007054550A1 (en) 2005-11-11 2007-05-18 Boehringer Ingelheim International Gmbh Quinazoline derivatives for the treatment of cancer diseases
PT1981863E (pt) 2006-01-26 2012-12-07 Boehringer Ingelheim Int Processo para preparar derivados de quinazolina substituídos por aminocrotonilamino
DK2068880T3 (da) 2006-09-18 2012-07-23 Boehringer Ingelheim Int Fremgangsmåde til behandling af cancer, der huser EGFR-mutationer
UY31867A (es) 2008-06-06 2010-01-29 Boehringer Ingelheim Int Nuevas formulaciones farmacéuticas sólidas que comprenden bibw 2992
TWI385174B (zh) 2008-11-10 2013-02-11 Nat Health Research Institutes 作為酪胺酸激酶抑制劑之稠合雙環及多環嘧啶化合物
SI2451445T1 (sl) 2009-07-06 2019-07-31 Boehringer Ingelheim International Gmbh Postopek za sušenje BIBW2992, njegovih soli in trdnih farmacevtskih formulacij, ki obsegajo to aktivno sestavino
US8828391B2 (en) 2011-05-17 2014-09-09 Boehringer Ingelheim International Gmbh Method for EGFR directed combination treatment of non-small cell lung cancer
CN103254183B (zh) * 2013-05-10 2015-11-11 苏州明锐医药科技有限公司 阿法替尼的制备方法
WO2014180271A1 (zh) * 2013-05-10 2014-11-13 苏州明锐医药科技有限公司 阿法替尼及其中间体的制备方法
ES2773296T3 (es) * 2013-10-23 2020-07-10 Gemvax & Kael Co Ltd Composición para tratar y prevenir la hiperplasia prostática benigna
US9242965B2 (en) 2013-12-31 2016-01-26 Boehringer Ingelheim International Gmbh Process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form and use thereof for synthesis of EGFR tyrosine kinase inhibitors
AU2016333987A1 (en) 2015-10-05 2018-05-10 Ny State Psychiatric Institute Activators of autophagic flux and phospholipase D and clearance of protein aggregates including tau and treatment of proteinopathies
CN105669658B (zh) * 2016-04-05 2018-06-29 北京民康百草医药科技有限公司 一种阿法替尼的精制方法
CN107488172B (zh) * 2016-06-10 2020-06-12 山东新时代药业有限公司 一种阿法替尼的制备方法

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